Article
The gatekeeper residue controls autoactivation of ERK2 via a pathway of intramolecular connectivity.
Proceedings of the National Academy of Sciences of the United States of America - 28 Nov 2006
Emrick Michelle A, Lee Thomas, Starkey Paul J, Mumby Marc C, Resing Katheryn A, Ahn Natalie G
Abstract excerpt
Studies of protein kinases have identified a "gatekeeper" residue, which confers selectivity for binding nucleotides and small-molecule inhibitors. We report that, in the MAP kinase ERK2, mutations at the gatekeeper residue unexpectedly lead to autoactivation due to enhanced autophosphorylation of regulatory Tyr and Thr sites within the activation lip that control kinase activity. This occurs through an...
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